American Chemical Society
tz2c00529_si_001.cif (432.32 kB)

A Photoactivatable AIEgen for Selective Imaging and Killing of Estrogen Receptor-Positive Cells

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posted on 2022-08-18, 12:20 authored by Changhuo Xu, Hang Zou, Lianrui Hu, Hanchen Shen, Herman H. Y. Sung, Haitao Feng, Ryan T. K. Kwok, Jacky W. Y. Lam, Lei Zheng, Ben Zhong Tang
The development of fluorescent probes based on the skeletal structure of small-molecule targeted anticancer drugs is promising for biomedical applications because these probes generally show trackable fluorescence and connatural bioactivity inherited from the parental anticancer drugs. By mimicking a classic estrogen receptor (ER) antagonist, namely, tamoxifen, we herein design and synthesize a photoactivatable luminogen with aggregation-induced emission and medicinal benefits. The probe is weakly emissive when it is selectively internalized by estrogen receptor-positive cells. Under photoirradiation, its emission can be turned on to report the intracellular distribution. The cell viability assay suggests that the probe only exhibits cytotoxicity to ER-positive cells but negligible cytotoxicity to ER-negative cells. This study thus provides new access to targeted theranostic systems with photoactivity.